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化合物简介
Exisulind (tentative trade name Aptosyn) is an antineoplastic agent. It acts by inhibiting the enzyme cyclic guanosine monophosphate phosphodiesterase type 5 (EC 3.1.4.17). It is the sulfone derivative of sulindac, an NSAID. Unlike sulindac, it has known effects on prostaglandin synthesis. It was developed as the potential treatment of several conditions including familial adenomatous polyposis (FAP), precancerous sporadic colonic polyps, cervical dysplasia and the prevention of tumor recurrence in prostate and breast cancer. Exisulind inhibits the enzyme cGMP-PDE, overexpressed in precancerous and cancerous colorectal cells, and induces apoptosis in such cells with minimal effects on normal cells. This apoptotic effect is independent of COX-1 or COX-2 inhibition, p53, Bcl-2, or cell cycle arrest. Preclinical evidence suggests that exisulind also inhibits angiogenesis.
基本信息
CAS:59973-80-7
中文别名:
英文别名:2-[(3Z)-6-fluoro-2-methyl-3-[(4-methylsulfonylphenyl)methylidene]inden-1-yl]acetic acid;Sulindac Sulfone;
分子式:C20H17FO4S
分子量:372.41
精确质量:372.083
Psa:79.82
Logp:5.1124
中文别名:
英文别名:2-[(3Z)-6-fluoro-2-methyl-3-[(4-methylsulfonylphenyl)methylidene]inden-1-yl]acetic acid;Sulindac Sulfone;
分子式:C20H17FO4S
分子量:372.41
精确质量:372.083
Psa:79.82
Logp:5.1124
编号系统
MDL号:MFCD00871143
物化性质
熔点:248-250ºC
储存条件:-20ºC Freezer
储存条件:-20ºC Freezer
安全信息
WGK Germany:3
生产方法及用途
合成路线
上游原料
下游产品
图谱
Predict 1H proton NMR
